The DOI matches its Crossref record; 23 of the 23 references it cites were found in a registry or an index.
Discovery and Cocrystal Structure of Benzodiazepinedione HDM2 Antagonists That Activate p53 in Cells
Open accessAbstract
HDM2 binds to an alpha-helical transactivation domain of p53, inhibiting its tumor suppressive functions. A miniaturized thermal denaturation assay was used to screen chemical libraries, resulting in the discovery of a novel series of benzodiazepinedione antagonists of the HDM2-p53 interaction. The X-ray crystal structure of improved antagonists bound to HDM2 reveals their alpha-helix mimetic properties. These optimized molecules increase the transcription of p53 target genes and decrease proliferation of tumor cells expressing wild-type p53.
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Citations
Cites
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In Vivo Activation of the p53 Pathway by Small-Molecule Antagonists of MDM2
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Structure of the MDM2 Oncoprotein Bound to the p53 Tumor Suppressor Transactivation Domain
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TGF-ß Signaling in Fibroblasts Modulates the Oncogenic Potential of Adjacent Epithelia
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High-Density Miniaturized Thermal Shift Assays as a General Strategy for Drug Discovery
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Self-citationDesign of a synthetic Mdm2-binding mini protein that activates the p53 response in vivo
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Molecular Mechanism of the Interaction between MDM2 and p53
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Cited by
Small molecules, big targets: drug discovery faces the protein–protein interaction challenge
Scott, D. E., Bayly, A. R., Abell, C., & Skidmore, J. (2016) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2016.29 · Cited by 1,137
Lu, H., Zhou, Q., He, J., Jiang, Z., Peng, C., Tong, R., & Shi, J. (2020) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-020-00315-3 · Cited by 891
Awakening guardian angels: drugging the p53 pathway
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Inhibition of α-helix-mediated protein–protein interactions using designed molecules
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Ding, K., Lu, Y., Nikolovska-Coleska, Z., Wang, G., Qiu, S., Shangary, S., Gao, W., Qin, D., Stuckey, J., Krajewski, K., et al. (2006) · Journal of Medicinal Chemistry · doi:10.1021/jm051122a · Cited by 702
Metadata
- Authors
- Grasberger, B. L., Lu, T., Schubert, C., Parks, D. J., Carver, T. E., Koblish, H. K., Cummings, M. D., LaFrance, L. V., Milkiewicz, K. L., Calvo, R. R., Maguire, D., Lattanze, J., Franks, C. F., Zhao, S., Ramachandren, K., Bylebyl, G. R., Zhang, M., Manthey, C. L., Petrella, E. C., Pantoliano, M. W., Deckman, I. C., Spurlino, J. C., Maroney, A. C., Tomczuk, B. E., Molloy, C. J., & Bone, R. F.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2005-02-01
- Volume
- 48
- Issue
- 4
- Pages
- 909-912
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2155782154
- Cited by
- 432
- References
- 23
- FWCI
- 11.31
- Type
- journal article
- Language
- en
- Open access
- green
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- Grasberger, B. L., Lu, T., Schubert, C., Parks, D. J., Carver, T. E., Koblish, H. K., Cummings, M. D., LaFrance, L. V., Milkiewicz, K. L., Calvo, R. R., Maguire, D., Lattanze, J., Franks, C. F., Zhao, S., Ramachandren, K., Bylebyl, G. R., Zhang, M., Manthey, C. L., Petrella, E. C., . . . Bone, R. F. (2005). Discovery and Cocrystal Structure of Benzodiazepinedione HDM2 Antagonists That Activate p53 in Cells. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm049137g
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
